EP1242077A4 - Novel processes for making- and a new crystalline form of- leflunomide - Google Patents

Novel processes for making- and a new crystalline form of- leflunomide

Info

Publication number
EP1242077A4
EP1242077A4 EP00989253A EP00989253A EP1242077A4 EP 1242077 A4 EP1242077 A4 EP 1242077A4 EP 00989253 A EP00989253 A EP 00989253A EP 00989253 A EP00989253 A EP 00989253A EP 1242077 A4 EP1242077 A4 EP 1242077A4
Authority
EP
European Patent Office
Prior art keywords
leflunomide
making
crystalline form
new crystalline
novel processes
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP00989253A
Other languages
German (de)
French (fr)
Other versions
EP1242077A1 (en
Inventor
Ilya Avrutov
Neomi Gershon
Judith Aronhime
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Teva Pharmaceutical Industries Ltd
Original Assignee
Teva Pharmaceutical Industries Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Teva Pharmaceutical Industries Ltd filed Critical Teva Pharmaceutical Industries Ltd
Publication of EP1242077A1 publication Critical patent/EP1242077A1/en
Publication of EP1242077A4 publication Critical patent/EP1242077A4/en
Withdrawn legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Rheumatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicinal Preparation (AREA)
EP00989253A 1999-12-16 2000-12-14 Novel processes for making- and a new crystalline form of- leflunomide Withdrawn EP1242077A4 (en)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US17122899P 1999-12-16 1999-12-16
US17123799P 1999-12-16 1999-12-16
US171228P 1999-12-16
US171237P 1999-12-16
US18264700P 2000-02-15 2000-02-15
US182647P 2000-02-15
US20241600P 2000-05-08 2000-05-08
US202416P 2000-05-08
PCT/US2000/033866 WO2001043742A1 (en) 1999-12-16 2000-12-14 Novel processes for making- and a new crystalline form of- leflunomide

Publications (2)

Publication Number Publication Date
EP1242077A1 EP1242077A1 (en) 2002-09-25
EP1242077A4 true EP1242077A4 (en) 2006-01-04

Family

ID=27496942

Family Applications (1)

Application Number Title Priority Date Filing Date
EP00989253A Withdrawn EP1242077A4 (en) 1999-12-16 2000-12-14 Novel processes for making- and a new crystalline form of- leflunomide

Country Status (15)

Country Link
US (3) US6610718B2 (en)
EP (1) EP1242077A4 (en)
JP (1) JP2003517011A (en)
KR (1) KR20020067545A (en)
CN (1) CN1411373A (en)
AU (1) AU779931B2 (en)
CA (1) CA2397601A1 (en)
CZ (1) CZ20022000A3 (en)
HR (2) HRP20020521A2 (en)
HU (1) HUP0204069A3 (en)
IL (1) IL149792A0 (en)
PL (1) PL356243A1 (en)
SK (1) SK8332002A3 (en)
WO (1) WO2001043742A1 (en)
YU (1) YU45102A (en)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2150808T3 (en) * 1997-08-08 2000-12-01 Aventis Pharma Gmbh CRYSTALLINE FORM OF (4-TRIFLUOROMETIL) -ANILIDA ACID 5-METHYLISOXAZOLE-4-CARBOXILICO.
CN1411373A (en) * 1999-12-16 2003-04-16 特瓦制药工业有限公司 Novel processes for making-and new crystalline form of-leflunomide
WO2001051089A1 (en) * 2000-01-13 2001-07-19 Merck Patent Gmbh Pharmaceutical preparations containing 2-pyrrolidone as the dissolving intermediary
HUP0301865A3 (en) * 2000-02-15 2005-12-28 Teva Pharma A method for synthesizing leflunomide
US20050158371A1 (en) * 2002-02-12 2005-07-21 Sumitomo Pharmaceuticals Co., Ltd. Novel external agent
WO2006103506A1 (en) * 2005-03-31 2006-10-05 Ranbaxy Laboratories Limited Sertraline-containing pharmaceutical compositions and a process for preparation thereof
CN101563082A (en) * 2006-09-05 2009-10-21 窦德献 Composition and method for treating immune-mediated skin disorders
CN101143834B (en) * 2006-09-15 2010-09-08 欣凯医药化工中间体（上海）有限公司 Polymorphism for N-(4-trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide sodium salt and preparation method thereof
AU2008272685B2 (en) 2007-06-29 2013-04-18 Generics [Uk] Limited Process for introduction of hydroxyethoxy side chain in bosentan
EP2222649A2 (en) 2007-10-24 2010-09-01 Generics (UK) Limited Novel crystalline forms
JP5683276B2 (en) 2008-02-08 2015-03-11 ジェネリクス・［ユーケー］・リミテッド Method for producing bosentan
US8975402B2 (en) 2008-11-03 2015-03-10 Generics [Uk] Limited HPLC method for the analysis of bosetan and related substances and use of these substances as reference standards and markers
CN101817797B (en) * 2009-02-26 2013-04-10 江苏亚邦爱普森药业有限公司 Synthesizing method of high-purity 3-methyl-N-[4-(trifluoromethyl) phenyl]-4-isoxazol formamide
TWI665190B (en) 2013-11-15 2019-07-11 阿克比治療有限公司 Solid forms of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions, and uses thereof
US11801232B2 (en) * 2019-11-27 2023-10-31 Yale University Targeting of ARID1A-deficient cancers by inhibiting de novo pyrimidine synthesis pathway
CN112898215B (en) * 2021-02-04 2022-11-08 美罗药业股份有限公司 Preparation method of leflunomide crystal form I

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4351841A (en) * 1978-12-16 1982-09-28 Hoechst Aktiengesellschaft Pharmaceutical preparation and method of treatment
WO1995019169A2 (en) * 1994-01-07 1995-07-20 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancer using inhibitors of platelet derived growth factor receptor
EP0903345A1 (en) * 1997-08-08 1999-03-24 Hoechst Marion Roussel Deutschland GmbH Crystal form of N-(4-trifluoromethylphenyl)-5-methylisoxazole-4-carboxamid
WO2000050411A1 (en) * 1999-02-26 2000-08-31 Aventis Pharma Deutschland Gmbh Method crystallising n-(4-trifluoromethylphenyl)-5-methyl-isoxazole-4-carboxamide
WO2001060363A1 (en) * 2000-02-15 2001-08-23 Teva Pharmaceutical Industries Ltd. A method for synthesizing leflunomide

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Publication number Priority date Publication date Assignee Title
US5268382A (en) * 1985-09-27 1993-12-07 Hoechst Aktiengesellschaft Medicaments to combat autoimmune diseases, in particular systemic lupus erythematosus
DE3534440A1 (en) * 1985-09-27 1987-04-02 Hoechst Ag DRUGS AGAINST CHRONIC GRAFT VERSUS HOST DISEASES AND AUTO AUTO DISEASES, IN PARTICULAR SYSTEMIC LUPUS ERYTHEMATODES
GB8619432D0 (en) * 1986-08-08 1986-09-17 Lilly Industries Ltd Pharmaceutical compounds
US5494911A (en) * 1990-05-18 1996-02-27 Hoechst Aktiengesellschaft Isoxazole-4-carboxamides and hydroxyalkylidenecyanoacetamides, pharmaceuticals containing these compounds and their use
US5610173A (en) * 1994-01-07 1997-03-11 Sugen, Inc. Formulations for lipophilic compounds
DE19610955A1 (en) * 1996-03-20 1997-09-25 Hoechst Ag Combination preparation containing 5-methylisoxazole-4-carboxylic acid- (4-trifluoromethyl) -anilide and N- (4-trifluoromethylphenyl) -2-cyano-3-hydroxycrotonic acid amide
GB9624038D0 (en) * 1996-11-19 1997-01-08 Sandoz Ltd Organic compounds
DE19711800A1 (en) * 1997-03-21 1998-09-24 Hoechst Ag Extension of expression of transgenic proteins by immunomodulating treatment
EP0933633A1 (en) * 1997-12-11 1999-08-04 Hoechst Marion Roussel Deutschland GmbH Process for obtaining L-dihydroorotic acid and use thereof
US7691890B2 (en) * 1998-03-11 2010-04-06 James W. Williams Anti-viral uses of leflunomide products
US6303652B1 (en) * 1998-08-21 2001-10-16 Hughes Institute BTK inhibitors and methods for their identification and use
US6248363B1 (en) * 1999-11-23 2001-06-19 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
CA2377278C (en) * 1999-06-25 2010-03-23 Vertex Pharmaceuticals Incorporated Prodrugs of carbamate inhibitors of impdh
CN1411373A (en) * 1999-12-16 2003-04-16 特瓦制药工业有限公司 Novel processes for making-and new crystalline form of-leflunomide
AU2001251011A1 (en) * 2000-03-27 2001-10-08 The General Hospital Corporation Treatments for immune-mediated ear disorders
AU2001284891A1 (en) * 2000-08-14 2002-02-25 Teva Pharmaceutical Industries Ltd. Micronized leflunomide
AU8523001A (en) * 2000-08-24 2002-03-04 Gtx Inc Selective androgen receptor modulators and methods of use thereof
JP4212278B2 (en) * 2001-03-01 2009-01-21 日本たばこ産業株式会社 Graft rejection inhibitor
US20040229849A1 (en) * 2002-09-24 2004-11-18 Jost-Price Edward Roydon Methods and reagents for the treatment of diseases and disorders associated with increased levels of proinflammatory cytokines
CA2535345A1 (en) * 2003-08-13 2005-03-03 Medtronic, Inc. Active agent delivery systems including a miscible polymer blend, medical devices, and methods
US20050064038A1 (en) * 2003-08-13 2005-03-24 Dinh Thomas Q. Active agent delivery systems including a single layer of a miscible polymer blend, medical devices, and methods
US20050053600A1 (en) * 2003-09-09 2005-03-10 Lane Thomas E. Methods for treating rheumatoid arthritis

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4351841A (en) * 1978-12-16 1982-09-28 Hoechst Aktiengesellschaft Pharmaceutical preparation and method of treatment
WO1995019169A2 (en) * 1994-01-07 1995-07-20 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancer using inhibitors of platelet derived growth factor receptor
EP0903345A1 (en) * 1997-08-08 1999-03-24 Hoechst Marion Roussel Deutschland GmbH Crystal form of N-(4-trifluoromethylphenyl)-5-methylisoxazole-4-carboxamid
WO2000050411A1 (en) * 1999-02-26 2000-08-31 Aventis Pharma Deutschland Gmbh Method crystallising n-(4-trifluoromethylphenyl)-5-methyl-isoxazole-4-carboxamide
WO2001060363A1 (en) * 2000-02-15 2001-08-23 Teva Pharmaceutical Industries Ltd. A method for synthesizing leflunomide

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
GUILLORY J K: "GENERATION OF POLYMORPHS, HYDRATES, SOLVATES, AND AMORPHOUS SOLIDS", POLYMORPHISM IN PHARMACEUTICAL SOLIDS, XX, XX, 1999, pages I - II,183, XP002350313 *
See also references of WO0143742A1 *

Also Published As

Publication number Publication date
HRP20050176A2 (en) 2005-08-31
HRP20020521A2 (en) 2004-08-31
HUP0204069A2 (en) 2003-04-28
WO2001043742A1 (en) 2001-06-21
US6610718B2 (en) 2003-08-26
AU2578801A (en) 2001-06-25
PL356243A1 (en) 2004-06-28
US20030203952A1 (en) 2003-10-30
AU779931B2 (en) 2005-02-17
SK8332002A3 (en) 2003-04-01
US6806373B2 (en) 2004-10-19
HUP0204069A3 (en) 2005-01-28
IL149792A0 (en) 2002-11-10
CZ20022000A3 (en) 2003-02-12
US20050004191A1 (en) 2005-01-06
YU45102A (en) 2006-01-16
CA2397601A1 (en) 2001-06-21
US20010031878A1 (en) 2001-10-18
EP1242077A1 (en) 2002-09-25
CN1411373A (en) 2003-04-16
KR20020067545A (en) 2002-08-22
JP2003517011A (en) 2003-05-20

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Legal Events

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